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首页> 外文期刊>Chemistry of heterocyclic compounds >Synthesis and inhibitory activity of 1,3-(adamantan-1(2)-yl)- imidazolidine-2,4,5-triones and 3,3'-(adamantan-1-yl)- bis(1-alkylimidazolidine-2,4,5-triones)
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Synthesis and inhibitory activity of 1,3-(adamantan-1(2)-yl)- imidazolidine-2,4,5-triones and 3,3'-(adamantan-1-yl)- bis(1-alkylimidazolidine-2,4,5-triones)

机译:1,3-(亚丹坦-1(2) - 基 - 咪唑烷-2,4,5-三&3,3' - (1-烷基咪唑烷-2,4,5-三酮)的合成和抑制活性

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摘要

A series of 1,3-(adamantan-1(2)-yl)imidazolidine-2,4,5-triones and 1,1'-(alkane-1,n-diyl)bis[3-(adamantan-1-yl)imidazolidine-2,4,5-triones] was synthesized via cyclization of 1,3-bis[adamantan-1(2)-ylureas] and 1,1'-(alkyl-1,n-diyl)bis[3-(adamantan-1-yl)ureas] with oxalyl chloride under mild conditions with high yields. All synthesized compounds were tested in vitro as inhibitors of soluble human epoxide hydrolase. A number of compounds have high inhibitory activity (IC50 1.6-650 nM), which makes them promising inhibitors of soluble epoxide hydrolase.
机译:一系列1,3-(Adamantan-1(2) - 基 - 基咪唑烷-2,4,5- Triones和1,1' - (烷烃-1,N-二基)BIS [3-(Adamantan-1- 通过1,3-双烷基-1(2) - 脲脲]和1,1' - (烷基-1,N-二基)BIS [3 - (Adamantan-1-Y1)尿布,在温和条件下具有高产率的草酰氯。 作为可溶性人环氧化物水解酶的抑制剂,在体外测试所有合成的化合物。 许多化合物具有高抑制活性(IC50 1.6-650nm),这使得它们具有可溶性环氧化物水解酶的有前途抑制剂。

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